BLZ945 | CSF-1R inhibitor

CAS:
 953769-46-5
Catalog Number:
 10-4979
BLZ945 chemical structure

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BLZ945 (953769-46-5) is a potent and brain-penetrant CSF-1R inhibitor (IC50 = 1 nM).1 It displayed significant antitumor effects in glioblastoma cells by altering the polarization of tumor-associated macrophages (TAMs). BLZ945 was shown to have significant antitumor effects in various cancer models via decreasing or reprogramming myeloid suppressor cells.2,3,4 It reversed the epithelial to mesenchymal transition in an inflammatory breast cancer model.5 BLZ945 modulated the tumor microenvironment in a lung cancer model by activating cross-talk between natural killer, T, and dendritic cells promoting antitumor immunity.6

References/Citations:

  1. Pyonteck et al. (2013), CSF-1R inhibition alters macrophage polarization and blocks glioma progression; Nat. Med. 19 1264
  2. Mao et al. (2016); Targeting Suppressive Myeloid Cells Potentiates Checkpoint Inhibitors to Control Spontaneous Neuroblastoma, Clin. Cancer Res. 22 3849
  3. Eissler et al. (2016); Regulation of myeloid cells by activated T cells determines the efficacy of PD-1 blockade, Oncoimmunology 5 e1232222
  4. Zhang et al. (2025); A CSF-1R inhibitor both prevents and treats triple-negative breast cancer brain metastases in hematogenous preclinical models, Clin. Exp. Metastasis 42 45
  5. Kai et al. (2018); CSF-1/CSF-1R axis is associated with epithelial/mesenchymal hybrid phenotype in epithelial-like inflammatory breast cancer, Sci. Rep. 8 9427
  6. Pfirschke et al. (2022); Macrophage-Targeted Therapy Unlocks Antitumoral Cross-talk between IFNγ-Secreting Lymphocytes and IL12-Producing Dendritic Cells, Cancer Immunol. Res. 10 40
953769-46-5, BLZ945, BLZ945 supplier, CSF-1R inhibitor, sotuletinib, Sotuletinib supplier
CAS:
953769-46-5
Catalog Number:
10-4979
Activity:
CSF-1R inhibitor
Chemical Names:
4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-1,3-benzothiazol-6-yl]oxy]-N-methylpyridine-2-carboxamide
Alternate Name:
Sotuletinib
Molecular Weight:
398.48
Molecular Formula:

C20H22N4O3S

Solubility:
Soluble in DMSO (>50 mg/ml)
Physical Properties:
Tan solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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BLZ945 (953769-46-5) is a potent and brain-penetrant CSF-1R inhibitor (IC50 = 1 nM).1 It displayed significant antitumor effects in glioblastoma cells by altering the polarization of tumor-associated macrophages (TAMs). BLZ945 was shown to have significant antitumor effects in various cancer models via decreasing or reprogramming myeloid suppressor cells.2,3,4 It reversed the epithelial to mesenchymal transition in an inflammatory breast cancer model.5 BLZ945 modulated the tumor microenvironment in a lung cancer model by activating cross-talk between natural killer, T, and dendritic cells promoting antitumor immunity.6

References/Citations:

  1. Pyonteck et al. (2013), CSF-1R inhibition alters macrophage polarization and blocks glioma progression; Nat. Med. 19 1264
  2. Mao et al. (2016); Targeting Suppressive Myeloid Cells Potentiates Checkpoint Inhibitors to Control Spontaneous Neuroblastoma, Clin. Cancer Res. 22 3849
  3. Eissler et al. (2016); Regulation of myeloid cells by activated T cells determines the efficacy of PD-1 blockade, Oncoimmunology 5 e1232222
  4. Zhang et al. (2025); A CSF-1R inhibitor both prevents and treats triple-negative breast cancer brain metastases in hematogenous preclinical models, Clin. Exp. Metastasis 42 45
  5. Kai et al. (2018); CSF-1/CSF-1R axis is associated with epithelial/mesenchymal hybrid phenotype in epithelial-like inflammatory breast cancer, Sci. Rep. 8 9427
  6. Pfirschke et al. (2022); Macrophage-Targeted Therapy Unlocks Antitumoral Cross-talk between IFNγ-Secreting Lymphocytes and IL12-Producing Dendritic Cells, Cancer Immunol. Res. 10 40

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